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A2AAR antagonist 4
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Catalog No. T212181
A2AAR antagonist 4 is an orally active antagonist of the A2A adenosine receptor (A2AAR) with a Ki value of 0.36 nM and a KB value of 1 nM in humans. At a concentration of 10 μM, it fully inhibits both human A2AAR and human A2bAR. A2AAR antagonist 4 is applicable in cancer research, such as studies involving MC38 tumors.
A2AAR antagonist 4
A2AAR antagonist 4
😃Good
Catalog No. T212181
A2AAR antagonist 4 is an orally active antagonist of the A2A adenosine receptor (A2AAR) with a Ki value of 0.36 nM and a KB value of 1 nM in humans. At a concentration of 10 μM, it fully inhibits both human A2AAR and human A2bAR. A2AAR antagonist 4 is applicable in cancer research, such as studies involving MC38 tumors.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
| Description | A2AAR antagonist 4 is an orally active antagonist of the A2A adenosine receptor (A2AAR) with a Ki value of 0.36 nM and a KB value of 1 nM in humans. At a concentration of 10 μM, it fully inhibits both human A2AAR and human A2bAR. A2AAR antagonist 4 is applicable in cancer research, such as studies involving MC38 tumors. |
| Targets&IC50 | A2B (human):85.8 nM (Ki) |
| In vitro | A2AAR antagonist 4 (Compound 4d) at a concentration of 10 μM completely inhibits hA2A AR, hA2B AR, and hA3 AR in the CHO-A2A cell line. Additionally, A2AAR antagonist 4, within the range of 0.1-1000 nM, restores IL-2 secretion in PBMC cells by fully displacing NECA, with an EC50 value of 2.06 nM. |
| In vivo | Compound 4d, an A2AAR antagonist, significantly inhibits tumor growth in MC38 tumor-bearing mice when administered at 100 mg/kg orally or 50 mg/kg via intraperitoneal injection, twice daily for 14 days. |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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